Combined use of chloramphenicol and zopiclone. Instructions for use of zopiclone. Release form and composition

A Zopiclone tablet contains 7.5 milligrams of the active drug compound of the same name. In addition, such auxiliary components as: microcrystalline cellulose, lactose monohydrate, potato starch, anhydrous colloidal silicon dioxide, magnesium stearate , and talc, aerosil and povidone .

Release form

This drug is produced in the form of tablets, on top of which a special coating is applied, as well as powder packaged in special sachets.

pharmachologic effect

The drug belongs to sedative and hypnotic drugs, members of the group pyrrolopyrazinamide .

Pharmacodynamics and pharmacokinetics

Since Zopiclone is hypnotic cyclopyrrolone derivative, the drug is effective agonists so-called benzodiazepine receptors . This medicine has a pronounced anxiolytic, and sedative effect . In addition, the drug stands out for its amnestic, anticonvulsant and muscle-relaxing properties.

Due to the chemical characteristics of the medicinal substance included in the preparation zopiclone , there is an increase GABAergic processes in the brain person, thereby increasing the threshold of sensitivity to GABA receptor mediator due to the interaction of active components with benzodiazepine receptors. Taking this medication reduces the number of times you wake up during the night.

In addition, the drug has a beneficial effect on the process of falling asleep and significantly increases the duration of sleep. It is worth noting that the drug does not have a negative effect on the sleep structure itself, i.e. does not change its stages, for example, does not reduce the duration of REM sleep, and so on. The drug dissolves quickly enough in stomach and reaches its maximum concentration after just a few hours after taking it.

The drug easily overcomes histohematic barrier and is evenly distributed in the tissues and organs of the human body, including the brain. When repeating a course of treatment with Zopiclone cumulation does not appear. Within half an hour after using the drug, a sound sleep occurs, the duration of which is a maximum of eight hours.

It is worth noting that when taking Zopiclone and drugs containing theophylline , patients with a significantly reduced duration, and, in addition, the intensity of asthmatic attacks in the pre-morning hours.

Indications for use

As a rule, the drug is prescribed for the following sleep disorders:

• difficulty falling asleep;
• constant night or morning awakenings;
• , including chronic, short-term or situational types of illness;
• restless sleep;
• sleep disorders associated with various types of mental disorders.

Contraindications

Absolute contraindications include:

• respiratory failure;
• age under 18 years;

In addition, patients with liver failure, at at malabsorption of galactose and glucose, with congenital galactosemia , at , and also at lactase deficiency .

Side effects

With the correct dosage of the drug, there are usually no side effects of Zopiclone. However, if the dosage is significantly exceeded, the following ailments may occur:

• behavioral disorders;
• aggressiveness;
• somnambulism;
• confusion or changes in consciousness;
• psychological or physiological dependence;
• speech disorders;
• lack of coordination;
• decreased sex drive;
• skin rashes;
• diplopia;
• hypotension;
• and other manifestations of allergies;
• asthenia;
• dispersion;
• hypotension;
• vomit;
• weight loss.

It is worth noting that in case of overdose, patients feel dry mouth and bitter taste . In some cases it may intensify liver enzyme activity .

Instructions for use of Zopiclone (Method and dosage)

The therapeutic (average) dose of the drug in accordance with the instructions for Zopiclone is 7.5 mg, which corresponds to one tablet. The medicine is taken immediately before bedtime. For severe forms insomnia the dosage can be doubled. However, elderly patients and people suffering from disorders liver functions should not take more than 3.75 mg. Zopiclone per day.

Overdose

An overdose of the drug occurs when the recommended average therapeutic doses of the drug are exceeded and can threaten the patient’s life. As a rule, in case of overdose occurs depression of the central nervous system (CNS). Signs of an overdose can be considered the patient's lethargic condition , and , confusion, respiratory depression, hypotension and hypotension.

If no more than an hour has passed since taking the drug, then you can call the patient vomiting . In other cases, you should immediately gastric lavage , while paying particular attention to the protection respiratory organs . In order to reduce absorption patients are prescribed zopiclone contained in the drug.

Pharmacological group: sleeping pills;
Systematic (IUPAC) name: (RS)-6-(5-chloropyridin-2-yl)-7-oxo-6,7-dihydro-5H-pyrrolopyrazin-5-yl-4-methylpiperazin-1-carboxylate
Trade names: Imovane, Zimovane
Legal status: Prescription only (Australia, UK, USA)
Application: oral tablets, 3.75 mg (UK), 5 or 7.5 mg
Bioavailability: 52-59% bound to plasma proteins
Metabolism: various liver cytochrome P450 enzymes
Half-life: ~6 hours
Excretion: urine
Formula: C 17 H 17 ClN 6 O 3
Mol. mass: 388.808 g/mol

Zopiclone (brand name Imovane in Canada, Australia, Sweden, Finland, Norway, Russia and the UK; brand name Zimovane in Europe) is a non-benzodiazepine hypnotic drug used in the treatment of insomnia. The substance is cyclopyrrolone, which increases normal transmission of the neurotransmitter GABA in the central nervous system, in the same way as benzodiazepines, but in a different way. Zopiclone is a sedative and is sold as a sleep aid. Its action is based on calming or suppressing the central nervous system. After prolonged use of zopiclone, tolerance and addiction to the drug may occur. When the dose is reduced or the drug is stopped, a withdrawal syndrome may develop, which may include a range of symptoms similar to those observed during benzodiazepine withdrawal. In the United States, zopiclone is not a commercially available drug, but its active stereoisomer, Eszopiclone, is sold under the brand name Lunesta. Zopiclone is under regulatory control in countries such as the United States, Japan, Brazil and some European countries. In these countries, possessing the drug without a prescription may be illegal. Zopiclone is also called the "Z-drug". Other Z-drugs include Zaleplon (Sonata) and Zolpidem (Ambien and AmbienCR). These drugs are considered less addictive than benzodiazepines. However, in recent years, reports of cases of dependence and addiction developing when taking Z-drugs have become more frequent. Zopiclone is recommended to be taken on a short-term basis, usually for a week or less. Daily or chronic use of the drug is usually not recommended.

Medical use

Zopiclone is used for the short-term treatment of insomnia in which the prominent symptoms include difficulty initiating or maintaining sleep. Long-term use of Zopiclone is not recommended, as tolerance and dependence may develop with prolonged use of the drug.

Elderly patients

Zopiclone, like other benzodiazepines and non-benzodiazepines, causes disturbances in body balance and standing stability in patients waking up at night or the next morning. Falls and hip fractures are frequently reported. Combination with alcohol increases the risk of such disorders. Partial, but incomplete, tolerance may develop towards such side effects. An extensive review of the medical literature regarding the treatment of insomnia in older adults found that there is sufficient evidence of the effectiveness and long-term benefits of non-drug treatments for insomnia. Compared with benzodiazepines, nonbenzodiazepine hypnotics and sedatives such as zopiclone offer few advantages in efficacy or tolerability in older adults. It has been found that new agents, such as melatonin agonists, may be more suitable and effective for the treatment of chronic insomnia in older adults. There is still insufficient evidence regarding the safety of long-term use of sedative hypnotics for insomnia. This use is not recommended for reasons that include concerns about possible adverse drug effects, including cognitive impairment (anterograde amnesia), daytime sedation, impaired motor coordination, and an increased risk of motor vehicle accidents and falls. In addition, the effectiveness and safety of long-term use of nonbenzodiazepine hypnotics remains to be determined. Further research is needed to evaluate the long-term effects of treatment and find the most appropriate treatment strategy for older adults with chronic insomnia.

Adverse reactions

The side effects most commonly observed in clinical trials were changes in taste or dysgeusia (a bitter, metallic taste in the mouth that goes away quickly in most users, but may persist until the drug's half-life has expired in some). After stopping the drug, you may experience heart palpitations during the daytime, especially after long periods of use. Zopiclone, like Triazolam and Rohypnol, causes memory impairment such as amnesia. The most significant side effect is impaired driving skills and an increased risk of traffic accidents. This side effect is not unique to Zopiclone and is also observed with other sleeping pills. A study evaluating the effects of zopiclone on next-day driving performance found that the drug's detrimental effect on driving performance was twice that of alcohol. Zaleplon does not have a detrimental effect on driving performance the day after use. Daytime anxiety associated with discontinuation of nonbenzodiazepines such as Zopiclone.

Common side effects

Gastrointestinal: taste disturbances, including a metallic taste and dry mouth. Nervous system: REM sleep disturbances, double vision, drowsiness, memory impairment, visuospatial disturbances, dizziness, headaches and fatigue. Unexpected mood changes are also possible, and if they occur, you should stop taking the drug immediately.

Less common side effects

Gastrointestinal: heartburn, constipation, diarrhea, nausea, coating on the tongue, bad breath, anorexia or increased appetite, vomiting, epigastric pain, dyspepsia, dehydration, paravgesia. Cardiovascular: palpitations in elderly patients. Skin: urticaria, tingling in the arms and legs. Miscellaneous: Blurred vision, frequent urination, nocturnal enuresis, mild to moderate increases in serum transaminases and/or alkaline phosphatase, and interstitial nephritis (very rare). Reproductive system: impotence, delayed ejaculation, anorgasmia in men and women. Nervous system: excitement, anxiety, memory loss, including anterograde and retrograde amnesia, confusion, dizziness, weakness, drowsiness, asthenia, euphoria and / or dysphoria, feeling of intoxication, depression, sleepwalking, coordination problems, hypotension, speech impairment, hallucinations , as a rule, auditory and visual, behavioral disorders, aggression, tremors, relapse of insomnia, nightmares, hypomania. Delirium is mainly observed in older people.

Tolerance, dependence and discontinuation

Zopiclone, a benzodiazepine-like drug, was initially presented as having a reduced risk of dependence and withdrawal symptoms compared with traditional benzodiazepine drugs. In reality, however, zopiclone may have an even slightly greater addiction potential than benzodiazepines. Tolerance to the effects of zopiclone may develop over several weeks. In most cases, long-term use of the drug should be avoided. Successful treatment of patients with severe insomnia due to anxiety can be achieved within a few months. Abrupt cessation of use, especially when taking high doses of the drug for a long time, can cause seizures and delirium in severe cases. Publications in the British Medical Journal provide no evidence that zopiclone has a low potential for addiction. In fact, physical dependence, abuse, and withdrawal symptoms similar to those observed with benzodiazepine withdrawal often occur with the drug. Symptoms of withdrawal syndrome include restlessness, tachycardia, tremors, sweating, hot flashes, palpitations, derealization, and later insomnia. Withdrawal seizures have also been reported during Zopiclone detoxification, however in this case the person was abusing high doses of Zopiclone. The risk of developing dependence when taking zopiclone for less than 2 weeks or less is very low. However, this is disputed by one study of low-dose zopiclone taken over 7 nights. Stopping zopiclone has been found to cause a relapse of insomnia. Additionally, when midazolam was discontinued after continuous use for 7 nights, no relapse of insomnia was observed, suggesting that zopiclone may cause more significant problems of tolerance and dependence than benzodiazepines. After 3 weeks of use, mild to moderate symptoms of relapse occur when zopiclone is stopped. Due to the risk of developing tolerance and physical dependence, zopiclone is recommended to be used for a short period of time (maximum 1-4 weeks), or, conversely, to rarely use the drug for long periods of time. Long-term users of Zopiclone who have become physically dependent on the drug should not abruptly stop taking the substance as severe withdrawal symptoms such as delirium may be associated with it. If zopiclone has been taken for several weeks or more, discontinuation of the drug should be done by gradually reducing the dose or switching to an equivalent dose (Valium), which has a much longer half-life, making withdrawal easier, and then gradually tapering over several months dosage to avoid the development of extremely severe and unpleasant withdrawal symptoms (such as internal restlessness, psychomotor agitation, abdominal pain, hypertension, hallucinations, seizures, anxiety, depression, psychosis, etc.), which can last up to two years if you stop taking the drug too abruptly. After 4 weeks of using zopiclone at night, some users develop daytime anxiety associated with stopping the drug. This symptom, however, does not occur as intensely as with triazolam, which has a much shorter duration of action and produces more severe symptoms of daytime withdrawal anxiety in long-term users. According to the World Health Organization, Zopiclone, although not molecularly a benzodiazepine, is capable of binding non-selectively and with high affinity to the same benzodiazepine binding site as benzodiazepines. The World Health Organization has also stated that zopiclone is cross-tolerant with benzodiazepines and these drugs can replace each other. A World Health Organization review of zopiclone found that the onset of withdrawal symptoms tends to occur either with excessive drug abuse or with long-term use of zopiclone. Zopiclone withdrawal symptoms include anxiety, tachycardia, tremors, sweating, relapse of insomnia, derealization, seizures, palpitations and hot flashes. Zopiclone is cross-tolerant with benzodiazepines. Alcohol exhibits cross-tolerance with positive GABA receptor modulators such as benzodiazepines and non-benzodiazepines. For this reason, alcoholics or recovering alcoholics may be at increased risk of physical dependence on zopiclone. In addition, alcoholics and drug abusers may be at increased risk of abuse and/or psychological dependence on zopiclone. Patients with alcoholism, drug abuse, or physical or psychological dependence on sedatives should avoid taking Zopiclone. Stopping Zopiclone is recommended by switching to an equivalent dose, as diazepam is available in low dosages, is cross-tolerant to zopiclone and lasts longer than zopiclone, allowing for a smoother withdrawal and allowing the body to adjust to a constant dose. Although Zopiclone acts at the same benzodiazepine receptors as drugs in the benzodiazepine family, it is not classified as a benzodiazepine (although it shares a number of characteristics and effects with them) due to differences in molecular structure. Zopiclone is classified as a cyclopyrrolone derivative.

Carcinogenicity

A recent analysis of US FDA data and clinical trial results suggests that non-benzodiazepine Z-drugs, at prescribed doses, are associated with an increased risk of cancer in humans. There were 15 epidemiological studies that showed that sleeping pills increased the risk of mortality, mainly due to increased mortality from cancer (brain, lung, bowel, breast and bladder). One possible explanation for the increase in cancer deaths is that Z-drugs have a negative effect on the immune system. The fact that increased disease rates were observed in clinical trials in patients taking other Z-drugs (zolpidem, zaleplon, and eszaleplon) may support this theory. Benzodiazepine sleeping pills are also associated with an increased risk of ovarian cancer. The development of malignant tumors has been associated with the use of zolpidem, but nothing can yet be said about the relationship of zolpidem with the development of neoplasms. Indiplon, another nonbenzodiazepine drug, also demonstrated an increased risk of cancer in clinical trials. The review concluded: "The risk of developing cancer is significant and physicians and patients should be aware that sleeping pills may increase a patient's risk of developing cancer."

Contraindications

Zopiclone causes decreased driving skills, similar to benzodiazepines. Long-term users of hypnotics develop only partial resistance to the adverse effects of the drugs associated with negative effects on driving skills. Users who take sleeping pills for an entire year are still at risk of road traffic accidents. You should avoid driving while taking Zopiclone. Zopiclone causes deterioration of psychomotor function. The day after taking Zopiclone, an effect such as deterioration in hand-eye coordination may occur. Patients with a history of drug abuse should avoid using Zopiclone as the substance has a very high abuse potential. Zopiclone can in some cases induce a state of amnesia associated with sleepwalking, which can progress to the point where the person is eating, interacting with people (quite convincingly), and even driving a car while actually asleep. Therefore, the drug is generally not used as a sedative (like benzodiazepines), since patients may make unfavorable decisions (as they are asleep) and engage in dangerous activities while the drug is active, without remembering any of this afterwards.

Special Precautions

Alcohol should be avoided when using zopiclone because alcohol and zopiclone enhance each other's effects, which may increase the risk of addiction. In patients with liver disease, zopiclone is eliminated from the body much more slowly than in normal patients. Such patients experience more pronounced pharmacological effects of the drug. Zopiclone reduces stability and increases the risk of falls in older adults, and also has cognitive side effects. Falls are one of the most common causes of death in older people. Patients suffering from muscle weakness as a result of myasthenia gravis, or having poor respiratory reserves due to severe chronic bronchitis, emphysema or other lung diseases, or experiencing sleep apnea, should avoid the use of Zopiclone. Patients with untreated thyroid disease should also avoid using the drug.

EEG and sleep

Like other sedative-hypnotics, zopiclone causes a decrease in body temperature and is effective in reducing sleep latency. Zopiclone causes benzodiazepine-like changes in EEG and sleep architecture, and also causes disturbances in sleep structure when discontinued, as a rebound effect. Zopiclone reduces delta waves and the number of high-amplitude delta waves, while increasing the number of low-amplitude waves. Zopiclone reduces the total amount of time in REM sleep and also delays the onset of REM sleep. Cognitive behavioral therapy is more effective in treating insomnia than zopiclone and has long-term effects on sleep quality for at least a year after therapy.

Pharmacology

Zopiclone acts as a hypnotic, anxiolytic, anticonvulsant, and muscle relaxant. Zopiclone and benzodiazepines act indiscriminately at the benzodiazepine-binding sites on the α1, α2, α3, and α5 GABA receptors as full agonists causing an increase in GABA action, resulting in the therapeutic and adverse effects of zopiclone. The metabolite of zopiclone is called desmethylzopiclone. The substance is also pharmacologically active and exhibits predominantly anxiolytic properties. Like benzodiazepines, zopiclone and its active metabolite desmethylzopiclone also inhibit N-methyl-D-aspartate (NMDA) receptors and nicotinic acetylcholine receptors, which may contribute to the addictive properties of these drugs. One study, however, demonstrated slight selectivity of zopiclone for the α1 and α5 subunits. It is believed, however, that zopiclone binds indiscriminately to the α1, α2, α3, and α5 GABA receptor benzodiazepine complexes. Desmethylzopiclone exhibits partial agonist properties, unlike zopiclone, which is a full agonist. The mechanism of action of zopiclone is similar to that of benzodiazepines, both substances have similar effects on motor activity and on the turnover of dopamine and serotonin. A meta-analysis of randomized controlled clinical trials comparing benzodiazepines and zopiclone or other Z-drugs such as zolpidem and zaleplon found that there were clear and consistent differences between zopiclone and benzodiazepines in terms of sleep onset latency, total sleep duration, number of awakenings, sleep quality, adverse effects, tolerance, relapse of insomnia and daytime activity. Zopiclone is part of the cyclopyrrolone family. Another drug in this class is Suriclone. Zopiclone, while molecularly different from benzodiazepines, has an almost identical pharmacological profile, including anxiolytic properties. It acts through binding to the benzodiazepine site as a full agonist, which in turn positively modulates benzodiazepine-sensitive GABA receptors and enhances GABA binding at these GABA receptors, providing the pharmacological action of Zopiclone. In addition to its pharmacological properties, Zopiclone may act similar to barbiturates. In EEG studies, zopiclone has been shown to significantly increase beta frequency band energy and show high voltage slow wave characteristics, desynchronization of hippocampal theta waves, and increased energy in the delta frequency band. Zopiclone increases both REM sleep and NREM sleep, while zolpidem, an α1-selective compound, increases only NREM sleep and has no effect on REM sleep. Zopiclone is less selective at the α1 site and has a higher affinity for the α2 site than zaleplon. Therefore, pharmacologically, Zopiclone is very similar to benzodiazepines.

Pharmacokinetics

After oral administration, zopiclone is rapidly absorbed, its bioavailability is about 80%. Plasma protein binding of zopiclone ranges from 45 to 80%. Zopiclone is rapidly and widely distributed into body tissues, including the brain, and is excreted in urine, saliva and breast milk. Zopiclone is partially metabolized in the liver to form an inactive N-demethylated derivative and its active N-oxide metabolite. In addition, approximately 50% of the administered dose is decarboxylated and excreted through the lungs. In urine, N-demethyl and N-oxide metabolites account for 30% of the initial dose. 7-10% of zopiclone is excreted from urine, indicating extensive metabolism of the drug prior to excretion. The terminal half-life (t1/2z) of zopiclone ranges from 3.5 to 6.5 hours. The pharmacokinetics of zopiclone in humans are stereoselective. Following oral administration of a racemic mixture, Cmax (time to maximum plasma concentration), AUC (area under the plasma time-concentration curve), and t1/2z values ​​are higher for the dextrorotatory enantiomer due to slower complete elimination and lower volume of distribution (adjusted). on bioavailability) compared to the levorotatory enantiomer. In urine, the concentrations of the dextrorotatory enantiomers of the N-demethyl and N-oxide metabolites are higher than the concentrations of the corresponding antipodes. The pharmacokinetics of zopiclone varies with age and is influenced by renal and hepatic function.

Interactions

Zopiclone also interacts with trimipramine and. Alcohol in combination with zopiclone increases its effects and adverse effects, including significantly increasing the potential for zopiclone overdose. |Erythromycin]] increases the rate of absorption of zopiclone and prolongs the half-life of zopiclone, which leads to increased plasma concentrations of the drug and more pronounced effects. Itraconazole has a similar effect on the pharmacokinetics of zopiclone. Older adults may be especially sensitive to drug interactions between itraconazole and zopiclone. A temporary dosage reduction may be necessary during combination therapy, especially in the elderly. Rifampicin causes a significant decrease in zopiclone half-life and peak plasma levels, resulting in a decrease in the hypnotic effects of zopiclone. Phenytoin and carbamazepine may also cause similar interactions. Ketoconazole and sulfaphenazole interfere with the metabolism of zopiclone. Nefazodone interferes with the metabolism of zopiclone, causing increased zopiclone levels and next-day sedation.

Story

Zopiclone was developed and first introduced in 1986 by Rhône-Poulenc S.A., now part of Sanofi-Aventis, the main manufacturer of Zopiclone worldwide. The drug was initially marketed as an improved version of benzodiazepines, but a recent meta-analysis showed that zopiclone has no particular advantage over benzodiazepines in any of the accrued aspects. On April 4, 2005, the US Drug Enforcement Administration designated zopiclone as a Schedule IV substance because the drug has addictive properties similar to benzodiazepines. Zopiclone, traditionally sold throughout the world, is a racemic mixture of two stereoisomers, only one of which is active. In 2005, the pharmaceutical company Sepracor of Marlborough, Massachusetts, began marketing the active stereoisomer of Eszopiclone under the name Lunesta in the United States. The consequence of this was the placement of this drug, which is a generic in most countries of the world, under patent control in the United States. Although the drug was expected to be available in generic form by 2010, no generic version of the drug has been brought to market to date. However, Zopiclone is currently available as a generic drug in several European countries, as well as in Brazil, Canada and Hong Kong. The difference between Eszopiclone and Zopiclone is the dosage - the most active dose of the Eszopiclone derivative contains 3 mg of the therapeutic stereoisomer, while the highest dose of zopiclone (7.5 mg) contains 3.75 mg of the active stereoisomer. These two substances have not yet been studied in comparative clinical trials to determine whether there are any potential clinical differences (in efficacy, side effects, dependence potential, safety, etc.)

Recreational use

Zopiclone is a drug that has the potential for abuse and drug escalation, drug addiction and drug dependence. Zopiclone is well known among drug addicts as an addictive drug. The drug is taken orally and sometimes intravenously and often in combination with alcohol to achieve a combined sedative-hypnotic-alcoholic euphoria. Patients who abuse the drug are at risk of developing dependence. After long-term use of the drug in normal doses, withdrawal symptoms may be observed, even after a gradual dose reduction. It is usually recommended to take Zopiclone no longer than 7-10 days, due to concerns about the possible development of dependence and tolerance to the drug. It is possible to develop two types of drug addiction: recreational abuse, when the drug is taken to achieve a “high,” or prolonged use of the drug without medical advice. Zopiclone may have a greater dependence potential than benzodiazepines. Patients with a history of substance abuse or psychiatric disorders may be at increased risk for abuse of high doses of Zopiclone. Symptoms of addiction from Zopiclone abuse may include depression, dysphoria, feelings of hopelessness, slowed thoughts, social isolation, anxiety, sexual anhedonia and nervousness. Zopiclone and other sedative-hypnotics are often found in cases where drivers are suspected of driving under the influence. Other drugs, including benzodiazepines and zolpidem, are also often found in such cases. In many drivers, blood levels of the drug significantly exceed the therapeutic dose and are often observed in combination with alcohol and other drugs. Benzodiazepines, zolpidem, and zopiclone are associated with a high risk of abuse. Zopiclone, which when taken in prescribed doses causes mild side effects observed the day after use, increases the risk of road traffic accidents by 50 percent. To reduce the risk of traffic accidents, it is recommended to use zaleplon or drugs instead of zopiclone. Zopiclone and other sleeping pills are sometimes used to commit criminal acts such as sexual assault. Zopiclone is cross-tolerant to barbiturates and may suppress signs of barbiturate withdrawal. Zopiclone is often used intravenously and has been shown in studies in monkeys to be associated with a high risk of abuse. Zopiclone is among the top ten drugs obtained using false prescriptions in France. However, due to the distinctly bitter taste of the drug, it is unlikely to be used for criminal purposes such as robbery and sexual assault. The tablets are coated with a special layer of film to mask the taste when swallowed, but this film is destroyed when chewed. Additionally, a common side effect is a bitter, metallic taste after ingestion, which is why a person taking zopiclone will likely know they are under the influence of the drug.

Overdose

Zopiclone is sometimes used as a method of suicide. Zopiclone has a mortality rate similar to benzodiazepines (except temazepam, which is toxic in overdose). Deaths have been reported due to overdose of Zopiclone, when taken alone or in combination with other drugs. An overdose of zopiclone may result in excessive sedation and decreased respiratory function, leading to coma and possibly death. Zopiclone in combination with alcohol, opiates, or other CNS depressants can lead to a fatal overdose. In case of an overdose of Zopiclone, you can take the benzodiazepine receptor antagonist flumazenil, which displaces zopiclone from the benzodiazepine binding site on the receptor, thereby helping to quickly eliminate the effects of zopiclone. Serious effects on the heart may also occur if Zopiclone is taken in combination with piperazine. Death certificates show an increase in Zopiclone overdose deaths. Zopiclone, when taken alone, is usually not fatal, but when combined with alcohol or other drugs such as opioids, or in patients with respiratory or liver disease, the risk of serious and fatal overdose increases.

Analogues (generics, synonyms)

No other names

Recipe (international)

Rp: Zopiclone 0.0075
D.t.d: N 5 in tab.
S: One tablet before bed

pharmachologic effect

A hypnotic from the group of cyclopyrrolones, which are structurally different from benzodiazepines and barbiturates. It has a sedative and hypnotic effect, which is due to a high degree of affinity for binding sites on the GABA receptor complex in the central nervous system. Quickly induces sleep without reducing the REM sleep phases in its structure, and then maintains sleep while maintaining normal phase composition. Does not cause post-somnia disorders: there are no feelings of weakness and drowsiness the next morning. Sleep occurs within 30 minutes and lasts 6-8 hours. Reduces headaches. In patients with nocturnal attacks of bronchial asthma, in combination with methylxanthine drugs (theophylline), it reduces asthma attacks in the early hours of the morning, reduces their intensity and duration.

Mode of application

For adults: Orally, 7.5 mg, 30-40 minutes before expected sleep, if necessary - up to 15 mg (maximum dose). The starting dose for the elderly and the maximum recommended dose for liver failure is 3.75 mg. Duration of continuous use - no more than 1 month.

Indications

Sleep disorders: difficulty falling asleep, night awakenings, early awakening; transient, situational and chronic insomnia; sleep disturbances in mental disorders, bronchial asthma with nocturnal attacks (in combination with a single daily dose of theophylline).

Contraindications

Hypersensitivity, severe respiratory failure, myasthenia gravis, severe liver failure, sleep apnea syndrome, age under 18 years, pregnancy, lactation. With caution. Liver failure.

Side effects

“Metallic” taste in the mouth, nausea, vomiting, mental disorders (irritability, confusion, depressed mood), allergic reactions (urticaria, rash). Upon awakening - drowsiness, dizziness, impaired coordination of movements, sometimes depressive states, aggressiveness, anterograde amnesia.

Release form

1 film-coated tablet contains zopiclone 7.5 mg and other excipients - lactose monohydrate, magnesium stearate, hypromellose, titanium dioxide, wheat starch, calcium dihydrogen phosphate, sodium salt of carboxymethyl starch; 10 pcs in a blister pack, 1 or 2 packs in a cardboard box.

ATTENTION!

The information on the page you are viewing is created for informational purposes only and does not in any way promote self-medication. The resource is intended to provide healthcare workers with additional information about certain medications, thereby increasing their level of professionalism. Use of the drug " Zopiclone“mandatorily requires consultation with a specialist, as well as his recommendations on the method of use and dosage of the medicine you have chosen.

International name

Zopiclone

Group affiliation

Sleeping pill

Dosage form

Tablets, film-coated tablets

pharmachologic effect

A hypnotic from the group of cyclopyrrolones, which are structurally different from benzodiazepines and barbiturates. It has a sedative and hypnotic effect, which is due to a high degree of affinity for binding sites on the GABA receptor complex in the central nervous system. Quickly induces sleep without reducing the REM sleep phases in its structure, and then maintains sleep while maintaining normal phase composition. Does not cause post-somnia disorders: there are no feelings of weakness and drowsiness the next morning.

Sleep occurs within 30 minutes and lasts 6-8 hours. Reduces headaches. In patients with nocturnal attacks of bronchial asthma, in combination with methylxanthine drugs (theophylline), it reduces asthma attacks in the early hours of the morning, reduces their intensity and duration.

Indications

Sleep disorders: difficulty falling asleep, night awakenings, early awakening; transient, situational and chronic insomnia; sleep disturbances in mental disorders, bronchial asthma with nocturnal attacks (in combination with a single daily dose of theophylline).

Contraindications

Hypersensitivity, severe respiratory failure, myasthenia gravis, severe liver failure, sleep apnea syndrome, age under 18 years, pregnancy, lactation. With caution. Liver failure.

Side effects

“Metallic” taste in the mouth, nausea, vomiting, mental disorders (irritability, confusion, depressed mood), allergic reactions (urticaria, rash).

Upon awakening - drowsiness, dizziness, impaired coordination of movements, sometimes depressive states, aggressiveness, anterograde amnesia.

Application and dosage

Orally, 7.5 mg, 30-40 minutes before expected sleep, if necessary, up to 15 mg (maximum dose). The starting dose for the elderly and the maximum recommended dose for liver failure is 3.75 mg. Duration of continuous use – no more than 1 month.

special instructions

Long-term use is not recommended (due to the possible development of drug dependence); the course of treatment should not exceed 4 weeks. Patients should drive a car and operate machinery with caution the day after taking the drug.

Interaction

Reduces plasma concentrations of trimipramine and its effect. Strengthens the effect of drugs that depress the central nervous system (including ethanol).

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Human sleep disturbance is considered a worldwide problem. The fatigue accumulated during the day literally knocks you off your feet. A man goes to bed and cannot sleep until the morning. A large number of people suffer from insomnia, and age practically does not matter in its onset. Teenagers and the elderly are susceptible to this disorder; even young children are not immune from it. Short-term manifestations of insomnia do not cause harm to the body. If sleep disturbance becomes chronic, a person’s quality of life and health suffers. That is why such a disorder must be dealt with in a timely manner. One of the drugs widely used for insomnia is Zopiclone. Instructions for use characterize it as excellent

Composition and release form

The drug is available in powder form for the preparation of dosage forms. The substance is packaged in double-layer plastic bags. The consumer can purchase the medicine at the pharmacy in tablet form. Its active component is the synthetic substance zopiclone. The instructions for use indicate that each tablet of the drug contains 7.5 mg of the active ingredient. The pills are packaged in blister packs.

Pharmacological properties

Zopiclone is a third-generation tranquilizer-hypnotic. Its main difference from other medications is its ability to maintain a complete sleep structure. The primary purpose of Zopiclone is to provide a hypnotic effect. Taking the medicine reduces the time it takes to fall asleep and significantly improves the quality of rest. In addition to sleeping pills, the medication has a relaxing and calming effect on the entire body.

Indications for use

What does the instructions for use say about the drug Zopiclone? According to the annotation, the medication helps you fall asleep quickly. It supports quality sleep at night by ensuring its phase composition. The medicine does not cause post-somnia disorders. This means that the next day there is no feeling of weakness or malaise.

Considering the described properties, Zopiclone is used for:

• sleep disorders (frequent awakenings, difficulty falling asleep);
• bronchial asthma with night awakenings;
• situational or chronic insomnia.

After taking the pill, sleep occurs within 30 minutes and lasts about 7-8 hours.

Directions for use and dosage regimen

The instructions for use of the drug "Zopiclone" recommend using it orally. The dosage regimen is determined by the doctor. As a rule, patients with insomnia are prescribed to take one tablet at night. If necessary, the dosage can be increased to two pills.

The tablets do not need to be chewed; it is better to take them with water. The effect of the drug begins 20-30 minutes after administration. The duration of the course of therapy should not exceed four weeks. Otherwise it develops which is very difficult to cope with. If, after one month, sleep does not return to normal, you need to consult a doctor again to adjust the treatment regimen.

Contraindications and side effects

In what cases should you refuse treatment with Zopiclone? The instructions do not recommend taking pills:

• pregnant and lactating women;
• children under 18 years of age;
• patients with respiratory failure.

The medication is prescribed with caution to people suffering from sleep apnea, acute liver or kidney failure.

The instructions for the drug prohibit its use during pregnancy. The active substance can provoke various disorders of the fetal central nervous system. In case of urgent need, the use of Zopiclone in the second trimester is allowed, but only with the permission of a doctor. During lactation, taking the medicine is possible provided that you stop breastfeeding for the entire duration of treatment.

If the Zopiclone dosage regimen is followed, the drug analogues are well tolerated by patients. In rare cases, excessive drowsiness and fatigue, dizziness and confusion may occur.

During treatment with Zopiclone, you should avoid drinking alcohol and medications that contain alcohol. Discontinuation of the drug must be carried out gradually. The risk of drug dependence, provided the medication is used for less than four weeks in a row, is minimal.

Cost of the product

What is the price of Zopiclone? The final cost of the drug depends on the markup of the pharmacy chain and the region of its location. On average, the price of one package ranges from 550 to 1000 rubles.

Analogues of the drug

Finding a good sleeping pill today is not difficult. Modern pharmaceutical companies offer many synonyms for the drug Zopiclone. Analogues differ only in cost and components.

The following drugs have a similar pharmacological effect on the body:

• "Hypnogen"
• "Andante".
• "Sanval."
• "Oniria."
• "Snovitel"

Common synonyms that contain a similar active ingredient include: “Imovan”, “Somnol”, “Thorson”.